Investigation of Interactions at the Extracellular Loops of the Relaxin Family Peptide Receptor 1 (RXFP1) [PDF]
Journal of Biological Chemistry, 2014 Relaxin, an emerging pharmaceutical treatment for acute heart failure, activates the relaxin family peptide receptor (RXFP1), which is a class A G-protein-coupled receptor. In addition to the classic transmembrane (TM) domain, RXFP1 possesses a large extracellular domain consisting of 10 leucine-rich repeats and an N-terminal low density lipoprotein ...
Catherine Z Chen +2 more
exaly +5 more sources
Engineering and Characterization of a Long-Half-Life Relaxin Receptor RXFP1 Agonist [PDF]
Molecular PharmaceuticsRelaxin-2 is a peptide hormone with important roles in human cardiovascular and reproductive biology. Its ability to activate cellular responses such as vasodilation, angiogenesis, and anti-inflammatory and antifibrotic effects has led to significant interest in using relaxin-2 as a therapeutic for heart failure and several fibrotic conditions. However,
Sarah C. Erlandson +5 more
europepmc +4 more sources
Proteomic and cytokine profiling of a CTRP8-RXFP1 glioma mouse model
Biochemical PharmacologyGlioblastoma (GB) is the most prevalent and aggressive primary brain tumor with fatal outcome due to a lack of effective treatments. We previously identified C1q-tumor necrosis factor-related protein 8 (CTRP8), a new member of the adiponectin family, as a novel agonist of the relaxin family peptide receptor 1 (RXFP1) and showed that the CTRP8-RXFP1 ...
Sabine Hombach-Klonisch, Thomas Klonisch
exaly +5 more sources
Expression of RXFP1 Is Decreased in Idiopathic Pulmonary Fibrosis: Implications for Relaxin-based Therapies [PDF]
American Journal of Respiratory and Critical Care Medicine, 2016 Abstract Rationale Relaxin is a hormone that has been considered as a potential therapy for patients with fibrotic diseases. Objectives To gauge the potential efficacy of relaxin-based therapies in idiopathic ...
John R Tedrow +2 more
exaly +5 more sources
Expression and function of G-protein-coupled receptorsin the male reproductive tract [PDF]
Anais da Academia Brasileira de Ciências, 2009 This review focuses on the expression and function of muscarinic acetylcholine receptors (mAChRs), α1-adrenoceptors and relaxin receptors in the male reproductive tract.
Maria Christina W. Avellar +2 more
doaj +5 more sources
RXFP1 Receptor Activation by Relaxin-2 Induces Vascular Relaxation in Mice via a Gαi2-Protein/PI3Kß/γ/Nitric Oxide-Coupled Pathway [PDF]
Frontiers in Physiology, 2018 Background: Relaxins are small peptide hormones, which are novel candidate molecules that play important roles in cardiometablic syndrome. Relaxins are structurally related to the insulin hormone superfamily, which provide vasodilatory effects by ...
Xiaoming Lian +6 more
doaj +2 more sources
Expression and Characterization of Relaxin Family Peptide Receptor 1 Variants [PDF]
Frontiers in Pharmacology, 2022 G-protein coupled receptors (GPCR) transduce extracellular stimuli into the cell interior and are thus centrally involved in almost all physiological-neuronal processes.
David Speck +11 more
doaj +3 more sources
Relaxin‐2 improves type I diabetes mellitus‐induced erectile dysfunction in rats by protecting cavernous endothelial and smooth muscle function, and inhibiting penile fibrosis and apoptosis [PDF]
Andrology, Volume 13, Issue 7, Page 1935-1946, October 2025.Abstract Background Diabetes mellitus‐induced erectile dysfunction (DMED) responds poorly to first‐line treatments, necessitating the development of new therapeutic strategies. Relaxin‐2 (RLX‐2) plays a crucial role in protecting vascular endothelium, vasodilatation, and antifibrosis in various diseases.
Bocheng Tu +10 more
wiley +2 more sources
Structural insights into G protein-coupled receptor signaling [PDF]
Structural DynamicsG protein-coupled receptors (GPCRs) are the largest single family of transmembrane proteins encoded in the human genome, and they are among the most successful classes of therapeutic drug targets of all time.
Andrew Kruse
doaj +2 more sources
Expression of relaxin-3 and its receptors in the hypothalamic-pituitary-ovary axis in layers and broiler breeders [PDF]
Poultry ScienceLayers can regulate their feed intake and maintain well-organized ovaries. Conversely, broiler breeders are prone to overeating, leading to disorganized ovaries.
Kahina Boukherroub +5 more
doaj +2 more sources